A method for the synthesis of fused chromeno quinolines by the palladium/copper cocatalyzed C-H bond activation and C-C bond cleavage reaction has been developed. A variety of fused chromeno quinoline derivatives could be synthesized by coumarin derivatives and anilines through the C-C bond cleavage/C-H functionalization/C-C bond formation process. The MTT assay was used to evaluate the chromeno quinolines against the human cervix tumor cells (HeLa), 3c and 9c without coordination metals showed good inhibition effect.